Drug intelligence / Profile preview

lutetium (177Lu) PSMA

Development stage
Preclinical
Lead developer
Novartis
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Lutetium-177 PSMA is a targeted radiopharmaceutical therapy developed by the Australian Nuclear Science and Technology Organisation (ANSTO) for the treatment of prostate cancer. The drug consists of the beta-emitting radioisotope Lutetium-177 (Lu-177) conjugated to a ligand that specifically targets Prostate-Specific Membrane Antigen (PSMA), a cell-surface protein that is highly overexpressed in prostate cancer cells, especially in metastatic and castration-resistant stages. Upon intravenous administration, the radioligand binds to PSMA-expressing tumor cells and is internalized via endocytosis. The Lu-177 isotope then emits high-energy beta particles with a short range (average 0.7 mm), which induce double-stranded DNA breaks and subsequent apoptosis in the target cells while minimizing radiation exposure to adjacent healthy tissues. ANSTO is a primary producer of high-purity, no-carrier-added (n.c.a.) Lu-177 and provides the finished radiopharmaceutical for various clinical trials and therapeutic applications in Australia.

Other names
Lutetium-177 PSMALutetium177 PSMALutetium 177 PSMAn.c.a. Lu-177 PSMAlutetium (177Lu) PSMA-617lutetium (177Lu) PSMA-I&T
02

Targets

PSMA (Prostate-specific membrane antigen)

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